pH敏感性薄膜包衣材料的合成及性质研究  

Synthesis and characterization of a novel pH-sensitive coating materials

作　　者：郑玲利[1] 黄园[1] 张志荣[1] 陈浮[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2005年第3期235-238,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家杰出青年科学基金资助项目(39925039)

摘　　要：目的制备pH4.0左右敏感的包衣材料,并研究其相关特性。方法用偏苯三酸酐和顺丁烯二酸酐对羟丙基甲基纤维素(HPMC)进行化学修饰,并对产物醋酸羟丙基甲基纤维素顺丁烯二酸酯(HPMCAM)和羟丙基甲基纤维素偏苯三甲酸酯(HPMCT)的性质(如pH敏感值、膜的透湿性)进行了初步研究。结果两类pH敏感的高分子材料成膜性良好,并具备药剂学薄膜衣材料的有关性质。HPMCT的pH敏感值为3.8～4.2,HPMCAM的pH敏感值为3.4～4.2。体外释放实验发现,HPMCAM与HPMCT制得的包衣片在人工胃液中2h未见药物释放,在pH4.0～4.2可迅速释药。结论HPMCAM与HPMCT可作为小肠上端十二指肠部位的药物定位释放包衣材料。OBJECTIVE To synthesize and characterizea pH-sensitive coating polymers which can dissolve at about pH 4.0. METHODS HPMC (hydroxypropyl methylcellulose) was chemically modified with maleic anhydrides and trimellic to obtain pH-sensitive HPMCAM (hydroxypropyl methylcellulose acetate maleate) and HPMCT (hydroxypropyl methylcellulose trimellitate) polymers. Pharmaceutical properties of HPMCAM and HPMCT such as pH-sensitive values, water vapor permeability were investigated. RESULTS The two kinds of materials showed good film forming property. The pH-sensitive values of HPMCT were 3.8 to 4.2, while those of HPMCAM are 3.4 to 4.2. In vitro results demonstratd that HPMCAM and HPMCT could suppress drug release completely within 2 hour in simulated gastric fluid (pH 1.2) and release the drug rapidly in phosphate buffer (pH 4.0～4.2). CONCLUSION These results indicate HPMCAM and HPMCT might be useful material for duodenum-specific drug delivery system.

关 键 词：薄膜包衣材料 PH敏感性 性质研究 羟丙基甲基纤维素 合成 体外释放实验 顺丁烯二酸 高分子材料 相关特性 化学修饰 药物释放 人工胃液 十二指肠 HPMC 甲酸酯 步研究 透湿性 成膜性 薄膜衣 药剂学 包衣片 

分 类 号：R971.1[医药卫生—药品] R944.9[医药卫生—药学]